Rocephin Actions

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Actions of Rocephin in details

infoThe action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease. Let us study what the actions of Rocephin drug is.

Pharmacology: Pharmacokinetics: Rocephin are nonlinear and all basic pharmacokinetic parameters, except the elimination half-life (t½), are dose dependent if based on total drug concentrations, increasing less than proportionally with dose. Non-linearity is due to saturation of plasma protein binding and is therefore observed for total plasma Rocephin but not for free (unbound) Rocephin.

Absorption: The maximum plasma concentration (Cmax) after a single IM dose of 1 g is about 81 mg/L and is reached in 2-3 hrs after administration. The area under the plasma concentration-time curve (AUC) after IM administration is equivalent to that after IV administration of an equivalent dose, indicating 100% bioavailability of IM administered Rocephin.

After IV bolus administration of 500 mg and 1 g, mean peak plasma Rocephin levels are approximately 120 and 200 mg/L. After IV infusion of Rocephin 500 mg, 1 g and 2 g, the plasma Rocephin levels are approximately 80, 150 and 250 mg/L respectively. Following IM injection, mean peak plasma Rocephin levels are approximately half those observed after intravenous administration of an equivalent dose.

Distribution: The volume of distribution of Rocephin is 7-12 L.

Rocephin has shown excellent tissue and body fluid penetration after a dose of 1-2 g; concentrations well above the minimal inhibitory concentrations of most pathogens responsible for infection are detectable for >24 hrs in over 60 tissues or body fluids including lung, heart, biliary tract/liver, tonsil, middle ear and nasal mucosa, bone as well as cerebrospinal, pleural, prostatic and synovial fluids.

On IV administration, Rocephin diffuses rapidly into the interstitial fluid, where bactericidal concentrations against susceptible organisms are maintained for 24 hrs.

Protein-Binding: Rocephin is reversibly bound to albumin. Plasma protein-binding is about 95% at plasma concentrations <100 mg/L. Binding is saturable and the bound portion decreases with rising concentration (up to 85% at a plasma concentration of 300 mg/L).

Penetration Into Particular Tissues: See figure.

Rocephin penetrates the meninges. Penetration is greatest when the meninges are inflamed. Mean peak Rocephin concentrations in cerebrospinal fluid (CSF) in patients with bacterial meningitis are reported to be up to 25% of plasma levels compared to 2% of plasma levels in patients with uninflammed meninges. Peak Rocephin concentrations in CSF are reached approximately 4-6 hrs after IV injection.

Rocephin crosses the placental barrier and is excreted in the breast milk at low concentrations.

Metabolism: Rocephin is not metabolised systematically; but is converted to inactive metabolites by the gut flora.

Elimination: Total plasma clearance is 10-22 mL/min. Renal clearance is 5-12 mL/min.

Fifty to sixty percent (50-60%) of Rocephin is excreted unchanged in the urine, while 40-50% is excreted unchanged in the bile. The elimination t½ in adults is about 8 hrs.

Special Populations: Children: The (t½) of Rocephin is prolonged in neonates. From 0-14 days of age, the levels of free Rocephin may be further increased by factors eg, reduced glomerular filtration and altered protein binding. During childhood, the (t½) is lower than in neonates or adults.

The plasma clearance and volume of distribution of total Rocephin are greater in neonates, infants and children than in adults.

Elderly: In elderly persons aged >75 years, the average elimination t½ is usually 2-3 times that of young adults.

Renal and Hepatic Impairment: In patients with renal or hepatic dysfunction, the pharmacokinetics of Rocephin are only minimally altered and the elimination t½ is only slightly increased, (<2 fold), even in patients with severely impaired renal function.

The modest increase in t½ in renal impairment is explained by a compensatory increase in non-renal clearance, resulting from a decrease in protein binding and corresponding increase in non-renal clearance of total Rocephin.

In patients with hepatic impairment, the elimination t½ of Rocephin is not increased, due to a compensatory increase in renal clearance. This is also due to an increase in plasma free fraction of Rocephin contributing to the observed paradoxical increase in total drug clearance, with an increase in volume of distribution paralleling that of total clearance.

Microbiology: The bactericidal activity of Rocephin results from inhibition of bacterial cell wall synthesis. Rocephin exerts in vitro activity against a wide range of gram-negative and gram-positive microorganisms. Rocephin is highly stable to most β-lactamases, both penicillinases and cephalosporinases, of gram-positive and gram-negative bacteria. Rocephin is usually active against the following microorganisms in vitro and in clinical infections.

Gram-Positive Aerobes: Staphylococcus aureus (methicillin-sensitive), Staphylococci coagulase-negative, Streptococcus pyogenes (β-hemolytic, group A), Streptococcus agalactiae (β-hemolytic, group B), β-hemolytic Streptococci (non-group A or B), Streptococcus viridans, Streptococcus pneumoniae.

Note: Methicillin-resistant Staphylococcus spp is resistant to cephalosporins, including Rocephin. In general, Enterococcus faecalis, Enterococcus faecium and Listeria monocytogenes are resistant.

Gram-Negative Aerobes: Acinetobacter lwoffi, Acinetobacter anitratus (mostly A. baumanii)*, Aeromonas hydrophila, Alcaligenes faecalis, Alcaligenes odorans, Alcaligenes-like bacteria, Borrelia burgdorferi, Capnocytophaga spp, Citrobacter diversus (including C. amalonaticus), Citrobacter freundii*, Escherichia coli, Enterobacter aerogenes*, Enterobacter cloacae*, Enterobacter spp (other)*, Haemophilus ducreyi, Haemophilus influenzae, Haemophilus parainfluenzae, Hafnia alvei, Klebsiella oxytoca, Klebsiella pneumoniae**, Moraxella catarrhalis (former Branhamella catarrhalis), Moraxella osloensis, Moraxella spp (other), Morganella morganii, Neisseria gonorrhea, Neisseria meningitidis, Pasteurella multocida, Plesiomonas shigelloides, Proteus mirabilis, Proteus penneri*, Proteus vulgaris*, Pseudomonas fluorescens*, Pseudomonas spp (other)*, Providentia rettgeri*, Providentia spp (other), Salmonella typhi, Salmonella spp (non-typhoid), Serratia marcescens*, Serratia spp (other)*, Shigella spp, Vibrio spp, Yersinia enterocolitica, Yersinia spp (other).

*Some isolates of these species are resistant to Rocephin, mainly due to the production of the chromosomally encoded ß-lactamase.

**Some isolates of these species are resistant due to production of extended spectrum, plasmid-mediated ß-lactamase.

Note: Many strains of the above micro-organisms that are multiple resistant to other antibiotics, eg, amino-penicillins and ureido-penicillins, older cephalosporins and aminoglycosides, are susceptible to Rocephin. Treponema pallidum is sensitive in vitro and in animal experiments. Clinical investigations indicate that primary and secondary syphilis respond well to Rocephin therapy. With a few exceptions clinical P. aeruginosa isolates are resistant to Rocephin.

Anaerobic Organisms: Bacteroides spp (bile-sensitive)*, Clostridium spp (excluding C. difficile), Fusobacterium nucleatum, Fusobacterium spp (other), Gaffkia anaerobica (formerly Peptococcus), Peptostreptococcus spp.

*Some isolates of these species are resistant to Rocephin due to ß lactamase production.

Note: Many strains of ß lactamase producing Bacteroides spp (notably B. fragilis) are resistant.

Clostridium difficile is resistant.

Susceptibility to Rocephin can be determined by the disk diffusion test or by the agar or broth dilution test using standardized techniques for susceptibility testing eg, those recommended by the National Committee for Clinical Laboratory Standards (NCCLS).

The NCCLS issued the following interpretative breakpoints for Rocephin: See Table 1.

Microorganisms should be tested with the Rocephin disk since it has been shown by in vitro tests to be active against certain strains resistant to cephalosporin class disks.

Where NCCLS recommendations are not in daily use, alternative, well-standardized, susceptibility-interpretative guidelines eg, those issued by DIN, ICS and others may be substituted.

Toxicology: Preclinical Safety Data: Teratogenicity: Reproductive studies in animals have shown no evidence of embryotoxicity, fetotoxicity, teratogenicity or adverse effects on male or female fertility, birth or perinatal and postnatal development. In primates, no embryotoxicity or teratogenicity has been observed.

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How should I take Rocephin?

A nurse or other trained health professional will give you this medicine. This medicine is given as a shot into one of your muscles or through a needle placed in one of your veins.

Rocephin administration

infoAdministration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route. The below information given tells about how Rocephin drug is administered.

Use exactly as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.

Rocephin is injected into a muscle, or into a vein through an IV. You may be shown how to use an IV at home. Do not self-inject this medicine if you do not fully understand how to give the injection and properly dispose of used needles, IV tubing, and other items used to inject the medicine.

Rocephin must be given slowly, and the IV infusion can take at least 30 minutes to complete.

You may need to mix Rocephin with a liquid (diluent) before using it. If you are using the injections at home, be sure you understand how to properly mix and store the medication. Use only the diluent your doctor has recommended.

After mixing your medicine, you will need to use it within a certain number of hours or days. This will depend on the diluent and how you store the mixture (at room temperature, in a refrigerator, or frozen). Carefully follow the mixing and storage instructions provided with your medicine. Ask your pharmacist if you have questions.

Do not mix Rocephin in the same injection with other antibiotics, or with any diluent that contains calcium, including a TPN (total parenteral nutrition) solution.

If you use other injectable medications, be sure to flush your intravenous catheter between injections of each medication.

Use this medicine for the full prescribed length of time. Your symptoms may improve before the infection is completely cleared. Skipping doses may also increase your risk of further infection that is resistant to antibiotics. Rocephin will not treat a viral infection such as the common cold or flu.

This medication can cause unusual results with certain lab tests for glucose (sugar) in the urine. Tell any doctor who treats you that you are using Rocephin.

Store unmixed Rocephin powder at room temperature, away from moisture, heat, and light.

If your medicine was provided in a frozen form or was frozen after mixing, thaw it in a refrigerator or at room temperature. Do not warm in a microwave or boiling water. Use the medicine as soon as possible after thawing it. Do not refreeze.

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Rocephin pharmacology

infoPharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body. Let us see the pharmacology for Rocephin drug.

Concretions consisting of the precipitated calcium salt of Rocephin have been found in the gallbladder bile of dogs and baboons treated with Rocephin.

These appeared as a gritty sediment in dogs that received 100 mg/kg/day for 4 weeks. A similar phenomenon has been observed in baboons but only after a protracted dosing period (6 months) at higher dose levels (335 mg/kg/day or more). The likelihood of this occurrence in humans is considered to be low, since Rocephin has a greater plasma half-life in humans, the calcium salt of Rocephin is more soluble in human gallbladder bile and the calcium content of human gallbladder bile is relatively low.

References

  1. EPA DSStox. "Ceftriaxone: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/dsstox... (accessed September 18, 2017).
  2. NCIt. "Cefuroxime: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser/Con... (accessed September 18, 2017).
  3. NCIt. "Ceftriaxone: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser/Con... (accessed September 18, 2017).

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The results of a survey conducted on ndrugs.com for Rocephin are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Rocephin. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.

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